An Open-label Phase 1/2A Study To Evaluate the Safety, Pharmacokinetics, Pharmacodynamics, and Preliminary Efficacy of TRC253, an Androgen Receptor Antagonist, in Patients With Metastatic Castration-resistant Prostate Cancer

This is a multi-center, first-in-human, open-label, Phase 1/2A dose-escalation study in which eligible patients with metastatic castration-resistant prostate carcinoma (mCRPC) will receive oral doses of TRC253. The study will be conducted in 2 parts: part 1 (dose escalation) and part 2 (dose expansion).

Start Date23 May 2017

Sponsor / Collaborator

TRACON Pharmaceuticals, Inc.

[+1]

100 Clinical Results associated with TRC-253

100 Translational Medicine associated with TRC-253

100 Patents (Medical) associated with TRC-253

Literatures (Medical) associated with TRC-253

12 Aug 2021·ACS medicinal chemistry lettersQ3 · MEDICINE

Spirocyclic Thiohydantoin Antagonists of F877L and Wild-Type Androgen Receptor for Castration-Resistant Prostate Cancer

Q3 · MEDICINE

Article

Author: Zhang, Zhuming ; Pande, Vineet ; Hickson, Ian ; Rocaboy, Christian ; Bignan, Gilles ; Trabalón Escolar, Luis ; Branch, Jonathan R. ; Lim, Heng-Keang ; Ondrus, Janine ; Bischoff, James R. ; Meerpoel, Lieven ; Connolly, Peter J. ; Bush, Tammy L.

Androgen receptor (AR) transcriptional reactivation plays a key role in the development and progression of lethal castration-resistant prostate cancer (CRPC). Recurrent alterations in the AR enable persistent AR pathway signaling and drive resistance to the treatment of second-generation antiandrogens. AR F877L, a point mutation in the ligand binding domain of the AR, was identified in patients who acquired resistance to enzalutamide or apalutamide. In parallel to our previous structure-activity relationship (SAR) studies of compound 4 (JNJ-pan-AR) and clinical stage compound 5 (JNJ-63576253), we discovered additional AR antagonists that provide opportunities for future development. Here we report a highly potent series of spirocyclic thiohydantoins as AR antagonists for the treatment of the F877L mutant and wild-type CRPC.

01 May 2021·Molecular cancer therapeutics

Discovery of JNJ-63576253, a Next-Generation Androgen Receptor Antagonist Active Against Wild-Type and Clinically Relevant Ligand Binding Domain Mutations in Metastatic Castration-Resistant Prostate Cancer

Article

Author: Gottardis, Marco M. ; Van Hecke, Geert ; Ondrus, Janine ; Packman, Kathryn ; Zhang, Zhuming ; Pande, Vineet ; Jaensch, Steffen ; Bischoff, James R. ; Parrett, Christopher J. ; Bignan, Gilles ; Branch, Jonathan R. ; Chong, Yolanda T. ; Bush, Tammy L. ; Habineza, Georges ; Meerpoel, Lieven ; Connolly, Peter J. ; Hickson, Ian

Abstract:

Numerous mechanisms of resistance arise in response to treatment with second-generation androgen receptor (AR) pathway inhibitors in metastatic castration-resistant prostate cancer (mCRPC). Among these, point mutations in the ligand binding domain can transform antagonists into agonists, driving the disease through activation of AR signaling. To address this unmet need, we report the discovery of JNJ-63576253, a next-generation AR pathway inhibitor that potently abrogates AR signaling in models of human prostate adenocarcinoma. JNJ-63576253 is advancing as a clinical candidate with potential effectiveness in the subset of patients who do not respond to or are progressing while on second-generation AR-targeted therapeutics.

28 Jan 2021·Journal of medicinal chemistryQ1 · MEDICINE

Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC)

Q1 · MEDICINE

Article

Author: Chong, Yolanda ; Meerpoel, Lieven ; Hickson, Ian ; Gottardis, Marco M. ; Ibrahim, Salam ; Teleha, Christopher ; Zhang, Zhuming ; Packman, Kathryn ; Pande, Vineet ; Luistro, Leopoldo ; Bignan, Gilles ; Branch, Jonathan R. ; Bush, Tammy ; Lim, Heng Keang ; Ondrus, Janine ; Bischoff, James R. ; Connolly, Peter J. ; Parrett, Christopher

Persistent androgen receptor (AR) activation drives therapeutic resistance to second-generation AR pathway inhibitors and contributes to the progression of advanced prostate cancer. One resistance mechanism is point mutations in the ligand binding domain of AR that can transform antagonists into agonists. The AR F877L mutation, identified in patients treated with enzalutamide or apalutamide, confers resistance to both enzalutamide and apalutamide. Compound 4 (JNJ-pan-AR) was identified as a pan-AR antagonist with potent activity against wild-type and clinically relevant AR mutations including F877L. Metabolite identification studies revealed a latent bioactivation pathway associated with 4. Subsequent lead optimization of 4 led to amelioration of this pathway and nomination of 5 (JNJ-63576253) as a clinical stage, next-generation AR antagonist for the treatment of castration-resistant prostate cancer (CRPC).

News (Medical) associated with TRC-253

16 Feb 2023

·www.prnewswire.com

DelveInsight Evaluates a Robust Prostate Cancer Pipeline as 170+ Influential Pharma Players to Set Foot in the Domain

Prostate cancer is the most common cancer in men and accounts for the second most cancer deaths among men globally. The rise in the number of cases of prostate cancer has led to growing government funding and rising initiatives by public and private organizations to spread awareness about prostate cancer. The emergence of strong pipeline drugs and the presence of novel prostate cancer treatments are the prominent factors that will escalate the growth rate of the prostate cancer therapeutics market. LAS VEGAS, Feb. 16, 2023 /PRNewswire/ -- DelveInsight's ' Prostate Cancer Pipeline Insight – 2023 ' report provides comprehensive global coverage of available, marketed, and pipeline prostate cancer therapies in various stages of clinical development, major pharmaceutical companies are working to advance the pipeline space and future growth potential of the prostate cancer pipeline domain. Key Takeaways from the Prostate Cancer Pipeline Report DelveInsight's prostate cancer pipeline report depicts a robust space with 170+ active players working to develop 200+ pipeline therapies for prostate cancer treatment. Key prostate cancer companies such as Merck & Co, Pfizer, Orion, Zenith Epigenetics, ESSA Pharma, RhoVac, AstraZeneca, Advaxis, Inc., Tracon Pharmaceuticals Inc., Bristol-Myers Squibb, Laekna Limited, Bracco Diagnostics, Inc, Arvinas Inc, Epizyme, Regeneron Pharmaceuticals, Veru Inc., Eli Lilly and Company, Exelixis, Luye Pharma Group, Amgen, Innocrin Pharmaceutical, Bayer, Nymox Pharmaceutical, Matrix Biomed, Tavanta Therapeutics, Fortis Therapeutics, Inc., Janssen Research & Development, LLC, Clarity Pharmaceuticals, Leap Therapeutics, Hinova pharmaceuticals, Vaccitech, Cardiff Oncology, Suzhou Kintor Pharmaceuticals, Teneobio, Inc., Janux Therapeutics, Fusion Pharmaceuticals, Corbus Pharmaceuticals, BioXcel Therapeutics, Onxeo S.A, Ayala Pharmaceuticals, HOOKIPA Pharma, Nuvation Bio, Ambrx, enGene, Jemincare, CellVax Therapeutics, POINT Biopharma, Oncternal Therapeutics, Immunic AG, BioNTech SE, and others are evaluating new prostate cancer drugs to improve the treatment landscape. Promising prostate cancer pipeline therapies in various stages of development include Pembrolizumab, Talazoparib, ODM-208, ZEN 3694, EPI-7386, RV 001, Adavosertib, Capivasertib, ADXS31-142, TRC253, Nivolumab, LAE001, BR55, ARV-110, Tazemetostat, REGN5678, VERU-111, Abemaciclib, Cabozantinib, LY01005, Tarlatamab, VT-464, BAY2315497, NX-1207, MBM-02, TAVT-45, FOR46, JNJ-78278343, 64Cu-SAR-bisPSMA, DKN-01, HC-1119, ChAdOx1-MVA 5T4, Onvansertib, GT0918, TNB-585, JANX007, 225Ac-PSMA I&T, CRB-701, BXCL701, AsiDNA, ADXS-504, HB-300, NUV-868, ARX517, JMKX002992, Zilovertamab, IMU-935, BNT112, and others. In February 2023, Fusion Pharmaceuticals announced the acquisition from RadioMedix, Inc. of the investigational new drug application for an ongoing Phase II clinical trial (the "TATCIST" trial) evaluating 225Ac-PSMA I&T, a small molecule targeting prostate-specific membrane antigen ("PSMA") expressed on prostate cancers. Following the closing, the alpha-emitting radiopharmaceutical being evaluated in the TATCIST trial will be known as FPI-2265. In February 2023, Corbus Pharmaceuticals entered into an exclusive licensing agreement with CSPC Megalith Biopharmaceutical Co., Ltd, a subsidiary of CSPC Pharmaceutical Group Limited for development and commercialization of CRB-701 (SYS6002): a novel clinical-stage antibody drug conjugate (ADC) targeting Nectin-4. The agreement covers exclusive commercialization rights to CRB-701 in the United States, Canada, the European Union (including the European Free Trade Area), the United Kingdom, and Australia. CSPC will retain all rights to SYS6002 in the remaining global markets. Clinical development is underway and will focus on urothelial cancer and other Nectin-4-positive solid tumors, potentially including lung, breast and prostate cancer. In February 2023, BioXcel Therapeutics, Inc.reported full data from its Phase IIa trial of BXCL701, the Company's investigational, oral innate immune activator, in combination with KEYTRUDA (pembrolizumab) in small cell neuroendocrine (SCNC) variant metastatic castration-resistant prostate cancer (mCRPC) patients after at least one prior line of chemotherapy for locally advanced or metastatic prostate cancer. Results will be presented in a rapid abstract presentation and a poster presentation at the 2023 American Society of Clinical Oncology Genitourinary Cancers (ASCO GU) Symposium on February 16, 2023. In January 2023, Onxeo S.A. gave an update on the clinical development program of its first-in-class drug candidate AsiDNA. Onxeo has activated its first US clinical study site, Next Oncology San Antonio. This phase I/II multicenter, basket trial intends to assess the safety and preliminary activity of AsiDNA in combination with olaparib in patients with recurrent ovarian, breast, and metastatic castration-resistant prostate cancer (mCRPC) who have progressed on previous PARP inhibitor therapy. In October 2022, Ayala Pharmaceuticals, Inc. and Advaxis, Inc. entered into a definitive merger agreement. The merger would result in a combined company that will focus predominantly on the development and commercialization of Ayala's lead program AL102 for the treatment of desmoid tumors and Advaxis's candidate ADXS-504 in development for prostate cancer. In October 2022, Janux Therapeutics announced that the first patient had been dosed in Phase I clinical trial of JANX007 in subjects with metastatic castration-resistant prostate cancer (mCRPC). JANX007 is a prostate-specific membrane antigen (PSMA) directed T cell engager (TCE) and is the first product candidate utilizing Janux's TRACTr platform to be administered in humans. Request a sample and discover the recent advances in prostate cancer drug treatment @ Prostate Cancer Pipeline Report The prostate cancer pipeline report provides detailed profiles of pipeline assets, a comparative analysis of clinical and non-clinical stage prostate cancer drugs, inactive and dormant assets, a comprehensive assessment of driving and restraining factors, and an assessment of opportunities and risks in the prostate cancer clinical trial landscape. Prostate Cancer Overview Prostate cancer is a type of cancer that arises from the prostate gland. It is the second leading cause of cancer death in men in the United States. 1 in every 9 men will be diagnosed with prostate cancer during their lifetime. Prostate cancer will be diagnosed in nearly 250,000 men this year. Breaking away from a prostate tumor allows prostate cancer cells to spread. They can spread to other body parts by passing through blood vessels or lymph nodes. Cancer cells that have spread may attach to other tissues and grow to form new tumors, causing damage wherever they land. Prostate cancer symptoms vary from person to person. Some men have no symptoms at all. Common prostate cancer symptoms include blood in the urine or semen, painful ejaculation, pain or burning during urination, and others. A biopsy is a primary tool for prostate cancer diagnosis, but a doctor can use other tools to ensure that the biopsy is performed in the correct location. Doctors may, for example, use transrectal ultrasound or magnetic resonance imaging (MRI) to guide the biopsy. Find out more about drugs for prostate cancer @ New Prostate Cancer Drugs A snapshot of the Prostate Cancer Pipeline Drugs mentioned in the report: Learn more about the emerging prostate cancer pipeline therapies @ Prostate Cancer Clinical Trials Prostate Cancer Therapeutics Assessment The prostate cancer pipeline report proffers an integral view of prostate cancer emerging novel therapies segmented by stage, product type, molecule type, mechanism of action, and route of administration. Scope of the Prostate Cancer Pipeline Report Coverage: Global Therapeutic Assessment By Product Type: Mono, Combination, Mono/Combination Therapeutic Assessment By Clinical Stages: Discovery, Pre-clinical, Phase I, Phase II, Phase III Therapeutics Assessment By Route of Administration: Oral, Parenteral, Intravenous, Subcutaneous, Topical Therapeutics Assessment By Molecule Type: Monoclonal Antibody, Peptides, Polymer, Small molecule, Gene therapy Therapeutics Assessment By Mechanism of Action: Programmed cell death-1 receptor antagonists, Poly(ADP-ribose) polymerase inhibitors, Proto oncogene protein c-akt inhibitors, Tubulin inhibitors; Tubulin polymerisation inhibitors, Antioxidants; Blood coagulation factor inhibitors; Inflammation mediator inhibitors; RNA replicase inhibitors, Bromodomain and extraterminal domain protein inhibitors, Immunostimulants, DNA topoisomerase I inhibitors, Androgen receptor antagonists, Polycomb repressive complex 2 inhibitors Key Companies: Merck & Co, Pfizer, Orion, Zenith Epigenetics, ESSA Pharma, RhoVac, AstraZeneca, Advaxis, Inc., Tracon Pharmaceuticals Inc., Bristol-Myers Squibb, Laekna Limited, Bracco Diagnostics, Inc, Arvinas Inc, Epizyme, Regeneron Pharmaceuticals, Veru Inc., Eli Lilly and Company, Exelixis, Luye Pharma Group, Amgen, Innocrin Pharmaceutical, Bayer, Nymox Pharmaceutical, Matrix Biomed, Tavanta Therapeutics, Fortis Therapeutics, Inc., Janssen Research & Development, LLC, Clarity Pharmaceuticals, Leap Therapeutics, Hinova pharmaceuticals, Vaccitech, Cardiff Oncology, Suzhou Kintor Pharmaceuticals, Teneobio, Inc., Janux Therapeutics, Fusion Pharmaceuticals, Corbus Pharmaceuticals, BioXcel Therapeutics, Onxeo S.A, Ayala Pharmaceuticals, HOOKIPA Pharma, Nuvation Bio, Ambrx, enGene, Jemincare, CellVax Therapeutics, POINT Biopharma, Oncternal Therapeutics, Immunic AG, BioNTech SE, and others. Key Prostate Cancer Pipeline Therapies: Pembrolizumab, Talazoparib, ODM-208, ZEN 3694, EPI-7386, RV 001, Adavosertib, Capivasertib, ADXS31-142, TRC253, Nivolumab, LAE001, BR55, ARV-110, Tazemetostat, REGN5678, VERU-111, Abemaciclib, Cabozantinib, LY01005, Tarlatamab, VT-464, BAY2315497, NX-1207, MBM-02, TAVT-45, FOR46, JNJ-78278343, 64Cu-SAR-bisPSMA, DKN-01, HC-1119, ChAdOx1-MVA 5T4, Onvansertib, GT0918, TNB-585, JANX007, 225Ac-PSMA I&T, CRB-701, BXCL701, AsiDNA, ADXS-504, HB-300, NUV-868, ARX517, JMKX002992, Zilovertamab, IMU-935, BNT112, and others. Dive deep into rich insights for new drugs for prostate cancer treatment; visit @ Prostate Cancer Medications Table of Contents For further information on the prostate cancer pipeline therapeutics, reach out @ Prostate Cancer Drug Treatment Related Reports Metastatic Prostate Cancer Pipeline Metastatic Prostate Cancer Pipeline Insight – 2023 report provides comprehensive insights about the pipeline landscape, including clinical and non-clinical stage products and the key metastatic prostate cancer companies, including Veru, Tracon, Sotio, among others. Metastatic Castration-Sensitive Prostate Cancer Pipeline Metastatic Castration-Sensitive Prostate Cancer Pipeline Insight – 2023 report provides comprehensive insights about the pipeline landscape, including clinical and non-clinical stage products, and the key metastatic castration-sensitive prostate cancer companies, including Merck, Pfizer, Veru, Tracon, Sotio, among others. Metastatic Hormone-Refractory Prostate Cancer Pipeline Metastatic Hormone-Refractory Prostate Cancer Pipeline Insight – 2023 report provides comprehensive insights about the pipeline landscape, including clinical and non-clinical stage products, and the key metastatic hormone-refractory prostate cancer companies, including Merck, Pfizer, Veru, Tracon, Sotio, among others. Metastatic Castration-Resistant Prostate Cancer Epidemiology Forecast Metastatic Castration-Resistant Prostate Cancer Epidemiology Forecast – 2032 report delivers an in-depth understanding of the disease, historical and forecasted epidemiology as well as the metastatic castration-resistant prostate cancer epidemiology trends. Metastatic Castration-Resistant Prostate Cancer Market Metastatic Castration-Resistant Prostate Cancer Market Insights, Epidemiology, and Market Forecast – 2032 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, market share of the individual therapies, and key metastatic castration-resistant prostate cancer companies including Zenith Epigenetics, Surface Oncology, Opna-IO LLC, Regeneron Pharmaceuticals, Veru Inc, among others. Other Trending Reports Tay-sachs Disease Or Gm2 Gangliosidosis Market | Onycholysis Market | Diagnostic Imaging Equipment Market | Chemotherapy-induced Peripheral Neuropathy Market | Global Electrophysiology Devices Market | Anaphylaxis Market | Atherectomy Devices Market | Helicobacter Pylori Infections Market | Ophthalmic Imaging Equipment Market | Androgenetic Alopecia Market | Allergic Rhinitis Market | Chronic Inflammatory Demyelinating Polyneuropathy Market | Chronic Inflammtory Demyelinating Polyneuropathy Market | Colorectal Cancer Crc Market | Opioid Induced Constipation Market | Vertigo Market | Bone Anchored Hearing Systems Market | Wound Closure Devices Market | Hip Replacement Devices Market | Hemodynamic Monitoring Systems Market | Egfr Non-small Cell Lung Cancer Market | Helicobacter Pylori Infection Market | Hyperkalemia Market | Polycythemia Market Neurostimulation Devices Market | Carpal Tunnel Syndrome Market | Ventilator Market | Cerebral Aneurysm Market | Alpha Antitrypsin Market | Binge Eating Disorder Market | Bunion Market | Concussions Market Size | Exocrine Pancreatic Insufficiency Market | Healthcare Due Diligence Services | Minimal Residual Disease Market | Hypertrophic Scar Market | Lung Fibrosis Market | Anterior Uveitis Market | 22q11.2 deletion syndrome Market | X-Linked Retinitis Pigmentosa (XLRP) Market | Acute Radiation Syndrome Market | Alpha-1 Protease Inhibitor Deficiency Market | Androgenetic Alopecia Market | Hyperlipidemia Market | Cardiotoxicity Market | Hypertrophic Cardiomyopathy Market | Fatty Acid Oxidation Disorders (FAODs) Market | Androgen Insensitivity Syndrome Market | Emphysema Market | Canaloplasty Market | Dravet Syndrome Market | Celiac Disease Market | Chlamydia Infections Market | Syphilis Market | Renal Tubular Acidosis Market | Palmoplantar Pustulosis (PPP) Market | Aplastic Anemia Market | Bacterial Pneumonia Market | B cell Chronic Lymphocytic Leukemia Market | B cell Lymphomas Market | Behcets Disease Market Neoantigen-based Personalized Cancer therapeutic Vaccines Competitive Landscape and Market Forecast—by 2035 | Glioblastoma Market Related Healthcare Blogs Metastatic Castration-Sensitive Prostate Cancer Market PARP Inhibitors for Metastatic Castration-Resistant Prostate Cancer Prostate Cancer Market Outlook Related Healthcare Services Healthcare Consulting Healthcare Competitive Intelligence Services Healthcare Asset Prioritization Services About DelveInsight DelveInsight is a leading Business Consultant and Market Research firm focused exclusively on life sciences. It supports pharma companies by providing comprehensive end-to-end solutions to improve their performance. Get hassle-free access to all the healthcare and pharma market research reports through our subscription-based platform PharmDelve . Connect with us on LinkedIn |Facebook|Twitter Additionally, get in touch with our business executive to explore @ Healthcare Due Diligence Services Contact Us Shruti Thakur [email protected] +1(919)321-6187 Logo: SOURCE DelveInsight Business Research, LLP

Phase 1Phase 2ASCO

05 May 2021

·www.globenewswire.com

TRACON Pharmaceuticals Reports First Quarter 2021 Financial

SAN DIEGO, May 05, 2021 (GLOBE NEWSWIRE) -- TRACON Pharmaceuticals (NASDAQ:TCON), a clinical stage biopharmaceutical company focused on the development and commercialization of novel targeted cancer therapeutics and utilizing a cost efficient, CRO-independent product development platform to partner with ex-U.S. companies to develop and commercialize innovative products in the U.S., today announced financial results for the first quarter ended March 31, 2021. The Company will host a conference call and webcast today at 4:30 PM Eastern Time / 1:30 PM Pacific Time. “We continue to be pleased with the pace of enrollment in the pivotal ENVASARC trial and remain on track to deliver interim data in the 2nd half of this year and final data in 2022,” said Charles Theuer, M.D., Ph.D., President and CEO of TRACON. “We have now initiated 22 sites and have enrolled more than 20 patients which has triggered the initial Data Monitoring Committee review of safety data from each cohort, which we expect later this quarter.” Recent Corporate Highlights Envafolimab Expected Key Upcoming Milestones First Quarter 2021 Financial Results Conference Call Details A live webcast of the conference call will be available online from the Investor/Events and Presentation page of the Company’s website at . After the live webcast, a replay will remain available on TRACON’s website for 60 days. About Envafolimab Envafolimab (KN035), a novel, single-domain antibody against PD-L1, is the first subcutaneously injected PD-(L)1 inhibitor to be studied in pivotal trials. Envafolimab is currently being studied in the ENVASARC Phase 2 pivotal trial in the U.S. sponsored by TRACON, has been studied in a completed Phase 2 pivotal trial as a single agent in MSI-H/dMMR advanced solid tumor patients in China and is being studied in an ongoing Phase 3 pivotal trial in combination with gemcitabine and oxaliplatin in advanced biliary tract cancer patients in China, with both Chinese trials sponsored by 3D Medicines. TRACON’s partners Alphamab Oncology and 3D Medicines submitted an NDA to the NMPA in China for envafolimab in MSI-H/dMMR cancer that was accepted for review in December 2020 and granted priority review in January 2021. In the Phase 2 MSI-H/dMMR advanced solid tumor trial, the confirmed objective response rate (ORR) by blinded independent central review in MSI-H/dMMR colorectal cancer (CRC) patients treated with envafolimab who failed a fluoropyrimidine, oxaliplatin and irinotecan was 32%, which was similar to the 28% confirmed ORR reported in the Opdivo package insert in MSI-H/dMMR CRC patients who failed a fluoropyrimidine, oxaliplatin, and irinotecan and the 33% confirmed ORR reported for Keytruda in MSI-H/dMMR CRC patients who failed a fluoropyrimidine, oxaliplatin and irinotecan in cohort A of the KEYNOTE-164 clinical trial. About ENVASARC (NCT04480502) The ENVASARC pivotal trial is a multi-center, open label, randomized, non-comparative, parallel cohort study at approximately 25 top cancer centers in the United States that began dosing in December 2020. TRACON expects the trial to enroll 160 patients with UPS or MFS who have progressed following one or two lines of prior treatment and have not received an immune checkpoint inhibitor, with 80 patients enrolled into cohort A of treatment with single agent envafolimab and 80 patients enrolled in cohort B of treatment with envafolimab and Yervoy. The primary endpoint is ORR by blinded independent central review with duration of response a key secondary endpoint. About TRC102 TRC102 (methoxyamine) is a novel, small molecule inhibitor of the DNA base excision repair pathway, which is a pathway that causes resistance to alkylating and antimetabolite chemotherapeutics. TRC102 is currently being studied in multiple Phase 1 and Phase 2 clinical trials sponsored by the National Cancer Institute through a Cooperative Research and Development Agreement (CRADA) and has orphan drug designation from the U.S. FDA in malignant glioma, including glioblastoma. About TJ004309 TJ004309 is a novel, humanized antibody against CD73, an ecto-enzyme expressed on stromal cells and tumors that converts extracellular adenosine monophosphate (AMP) to adenosine, which is highly immunosuppressive. TJ004309 is currently being studied in an ongoing Phase 1 trial to assess safety and preliminary efficacy as a single agent and when combined with the PD-L1 checkpoint inhibitor Tecentriq in patients with advanced solid tumors. About TRACON TRACON develops targeted therapies for cancer utilizing a capital efficient, CRO independent, product development platform. The Company’s clinical-stage pipeline includes: Envafolimab, a PD-L1 single-domain antibody given by rapid subcutaneous injection that is being studied in the pivotal ENVASARC trial for sarcoma; TRC253, a Phase 3 ready small molecule drug candidate for the treatment of prostate cancer; TRC102, a Phase 2 small molecule drug candidate for the treatment of lung cancer; and TJ004309, a CD73 antibody in Phase 1 development for the treatment of advanced solid tumors. TRACON is actively seeking additional corporate partnerships whereby it leads U.S. regulatory and clinical development and shares in the cost and risk of clinical development and leads U.S. commercialization. In these partnerships TRACON believes it can serve as a solution for companies without clinical and commercial capabilities in the U.S. To learn more about TRACON and its product pipeline, visit TRACON's website at . Forward-Looking Statements Statements made in this press release regarding matters that are not historical facts are “forward-looking statements” within the meaning of the Private Securities Litigation Reform Act of 1995. Because such statements are subject to risks and uncertainties, actual results may differ materially from those expressed or implied by such forward‐looking statements. Such statements include, but are not limited to, statements regarding TRACON's and its collaboration partners’ plans to further develop product candidates, expectations regarding the timing and scope of clinical trials and availability of clinical data, expected development, regulatory and commercial milestones and timing thereof, estimated cash runway, potential utility of product candidates, potential events under collaboration and license agreements, and TRACON’s business development strategy and goals to enter into additional collaborations. Risks that could cause actual results to differ from those expressed in these forward‐looking statements include: risks associated with clinical development and regulatory approval of novel pharmaceutical products; whether TRACON or others will be able to complete or initiate clinical trials on TRACON’s expected timelines, if at all, including due to risks associated with the COVID-19 pandemic; the fact that future preclinical studies and clinical trials may not be successful or otherwise consistent with results from prior studies; the fact that TRACON has limited control over whether or when third party collaborators complete on-going trials or initiate additional trials of TRACON’s product candidates; the fact that TRACON’s collaboration agreements are subject to early termination; whether TRACON will be able to enter into additional collaboration agreements on favorable terms or at all; potential changes in regulatory requirements in the United States and foreign countries; TRACON’s reliance on third parties for the development of its product candidates, including the conduct of its clinical trials and manufacture of its product candidates; whether TRACON will be able to obtain additional financing; the possibility of unexpected expenses or other uses of TRACON’s cash resources; and other risks described in TRACON’s filings with the Securities and Exchange Commission under the heading “Risk Factors”. All forward‐looking statements contained in this press release speak only as of the date on which they were made and are based on management’s assumptions and estimates as of such date. TRACON undertakes no obligation to update such statements to reflect events that occur or circumstances that exist after the date on which they were made. TRACON Pharmaceuticals, Inc.Unaudited Condensed Consolidated Statements of Operations(in thousands, except share and per share data) TRACON Pharmaceuticals, Inc.Unaudited Condensed Consolidated Balance Sheets(in thousands)

Financial StatementAntibodyOrphan DrugSmall molecular drugPriority Review

03 May 2021

·www.globenewswire.com

TRACON Pharmaceuticals Announces Appointment of Dongliang Zhuang, Ph.D. as Vice President of Statistics and Biometrics

SAN DIEGO, May 03, 2021 (GLOBE NEWSWIRE) -- TRACON Pharmaceuticals (NASDAQ: TCON), a clinical stage biopharmaceutical company focused on the development and commercialization of novel targeted cancer therapeutics and utilizing a cost efficient, CRO-independent product development platform to partner with ex-U.S. companies to develop and commercialize innovative products in the U.S., announced today the appointment of Dongliang Zhuang, Ph.D. as Vice President of Statistics and Biometrics. “We are very pleased to welcome Dongliang to the TRACON senior management team,” said Charles Theuer, M.D., Ph.D., President and CEO of TRACON. “His strong experience at the U.S. FDA and on BLA submissions at biopharmaceutical companies will be invaluable to TRACON as we execute on our plan to complete the ENVASARC trial and begin activities expected to culminate in a BLA for envafolimab based on ENVASARC data.” Dr. Zhuang brings more than two decades of broad statistical experience to TRACON. Following his time at the U.S. FDA, he served as the Head of Biostatistics and Programming at multiple biopharmaceutical companies. At Amylin, he was the project statistician for the development of the company’s leading diabetic product Bydureon including the pivotal trial that was the basis for FDA approval, and lead statistician for Byetta where he oversaw studies that supported the successful Byetta New Drug Application. “TRACON has a first-class management team, the efficient Product Development Platform of CRO-independent research to conduct global clinical trials, and a promising drug candidate with near-term commercial potential in envafolimab,” said Dr. Zhuang. “I am thrilled to support TRACON’s mission and oversee statistics and biometrics within its broad oncology pipeline, which has the potential to address significant unmet needs across multiple tumor types.” About Envafolimab Envafolimab (KN035), a novel, single-domain antibody against PD-L1, is the first subcutaneously injected PD-(L)1 inhibitor to be studied in pivotal trials. Envafolimab is currently being studied in the ENVASARC Phase 2 pivotal trial in the U.S. sponsored by TRACON, has been studied in a completed Phase 2 pivotal trial as a single agent in MSI-H/dMMR advanced solid tumor patients in China and is being studied in an ongoing Phase 3 pivotal trial in combination with gemcitabine and oxaliplatin in advanced biliary tract cancer patients in China, with both Chinese trials sponsored by 3D Medicines. TRACON’s partners Alphamab Oncology and 3D Medicines submitted an NDA to the NMPA in China for envafolimab in MSI-H/dMMR cancer that was accepted for review in December 2020 and granted priority review in January 2021. In the Phase 2 MSI-H/dMMR advanced solid tumor trial, the confirmed objective response rate (ORR) by blinded independent central review in MSI-H/dMMR colorectal cancer (CRC) patients treated with envafolimab who failed a fluoropyrimidine, oxaliplatin and irinotecan was 32%, which was similar to the 28% confirmed ORR reported in the Opdivo package insert in MSI-H/dMMR CRC patients who failed a fluoropyrimidine, oxaliplatin, and irinotecan and the 33% confirmed ORR reported for Keytruda in MSI-H/dMMR CRC patients who failed a fluoropyrimidine, oxaliplatin and irinotecan in cohort A of the KEYNOTE-164 clinical trial. About ENVASARC (NCT04480502) The ENVASARC pivotal trial is a multi-center, open label, randomized, non-comparative, parallel cohort study at approximately 25 top cancer centers in the United States that began dosing in December 2020. TRACON expects the trial to enroll 160 patients with UPS or MFS who have progressed following one or two lines of prior treatment and have not received an immune checkpoint inhibitor, with 80 patients enrolled into cohort A of treatment with single agent envafolimab and 80 patients enrolled in cohort B of treatment with envafolimab and Yervoy. The primary endpoint is ORR by blinded independent central review with duration of response a key secondary endpoint. About TRACON TRACON develops targeted therapies for cancer utilizing a capital efficient, CRO independent, product development platform. The Company’s clinical-stage pipeline includes: Envafolimab, a PD-L1 single-domain antibody given by rapid subcutaneous injection that is being studied in the pivotal ENVASARC trial for sarcoma; TRC253, a Phase 3 ready small molecule drug candidate for the treatment of prostate cancer; TRC102, a Phase 2 small molecule drug candidate for the treatment of lung cancer; and TJ004309, a CD73 antibody in Phase 1 development for the treatment of advanced solid tumors. TRACON is actively seeking additional corporate partnerships whereby it leads U.S. regulatory and clinical development and shares in the cost and risk of clinical development and leads U.S. commercialization. In these partnerships TRACON believes it can serve as a solution for companies without clinical and commercial capabilities in the U.S. To learn more about TRACON and its product pipeline, visit TRACON’s website at . Forward-Looking Statements Statements made in this press release regarding matters that are not historical facts are “forward-looking statements" within the meaning of the Private Securities Litigation Reform Act of 1995. Because such statements are subject to risks and uncertainties, actual results may differ materially from those expressed or implied by such forward‐looking statements. Such statements include, but are not limited to, statements regarding TRACON’s plans to further develop product candidates, expectations regarding the timing and scope of clinical trials, expected development and regulatory milestones and timing thereof, potential utility of product candidates, and TRACON’s business development and commercialization strategy and goals. Risks that could cause actual results to differ from those expressed in these forward‐looking statements include: risks associated with clinical development; whether TRACON or others will be able to complete or initiate clinical trials on expected timelines, if at all; potential guidance from the FDA regarding clinical development plans that is inconsistent with TRACON’s expectations; the fact that future preclinical studies and clinical trials may not be successful or otherwise consistent with results from prior studies; the fact that TRACON’s collaboration agreements are subject to early termination; whether or when envafolimab receives regulatory approval in the United States or is successfully commercialized; whether TRACON will be able to enter into additional collaboration agreements on favorable terms or at all; potential changes in regulatory requirements in the United States and foreign countries; TRACON’s reliance on third parties for the development of its product candidates, including the conduct of its clinical trials and manufacture of its product candidates; whether TRACON will be able to obtain additional financing; and other risks described in TRACON’s filings with the Securities and Exchange Commission under the heading “Risk Factors”. All forward‐looking statements contained in this press release speak only as of the date on which they were made and are based on management’s assumptions and estimates as of such date. TRACON undertakes no obligation to update such statements to reflect events that occur or circumstances that exist after the date on which they were made.

AntibodySmall molecular drugPriority Review

100 Deals associated with TRC-253

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Prostatic Cancer	Phase 2	US	Janssen Research & Development LLC	22 Mar 2021
Adenocarcinoma of prostate	Phase 2	US	Janssen Pharmaceutica NV	23 May 2017
Adenocarcinoma of prostate	Phase 2	US	TRACON Pharmaceuticals, Inc.	23 May 2017
Metastatic castration-resistant prostate cancer	Phase 2	US	TRACON Pharmaceuticals, Inc.	23 May 2017
Metastatic castration-resistant prostate cancer	Phase 2	US	Janssen Pharmaceutica NV	23 May 2017

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02987829 (CTgov)	Phase 1/2	Metastatic castration-resistant prostate cancer \| Adenocarcinoma of prostate	72	TRC253 (40 mg TRC253/Daily)	qygencthig(nnkyhfqvjg) = fcvtcyjgeo slbsqybbel (oeywrftjmu, xnxsotkmla - mfoeqgrtqp) View more	-	23 Apr 2021
NCT02987829 (CTgov)	Phase 1/2		72	TRC253 (80 mg TRC253/Daily)	qygencthig(nnkyhfqvjg) = owwsasvfel slbsqybbel (oeywrftjmu, kaliqgjzza - raebcothud) View more	-	23 Apr 2021
NCT02987829 (ASCO2019) Manual	Phase 1/2	Metastatic castration-resistant prostate cancer	22	TRC-253	svcyxbihpo(zlfhjmoicb) = One G3 QTcF prolongation at 320 mg eeotgdoylu (dsdydhyuld ) View more	Positive	31 May 2019

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